avanafil

avanafil

Stendra

Pharmacologic class: Phosphodiesterase type 5 (PDE5) inhibitor

Therapeutic class: Erectile dysfunction agent

Pregnancy risk category C

Action

Enhances the effect of nitric oxide by inhibiting PDE5, which is responsible for degradation of cyclic guanosine monophosphate in the corpus cavernosum. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 has no effect in the absence of sexual stimulation.

Availability

Tablets: 50 mg, 100 mg, 200 mg

Indications and dosages

➣ Erectile dysfunction

Adults: Initially, 100 mg P.O. approximately 30 minutes before sexual activity on an as-needed basis. May increase dosage to 200 mg or decrease to 50 mg based on efficacy or tolerability; use the lowest dosage that provides benefit. Not to exceed one dose daily.

Dosage adjustment

• Concurrent use of moderate CYP3A4 inhibitors

• Concurrent use of alpha blockers

Contraindications

• Hypersensitivity to drug or its components

• Concurrent use of any form of organic nitrates

Precautions

Use cautiously in:

• severe hepatic or renal impairment (avoid use)

• mild to moderate hepatic or renal impairment

• patients in whom sexual activity is inadvisable due to CV status (particularly those with left ventricular outflow obstruction, such as aortic stenosis or idiopathic hypertrophic subaortic stenosis, and those with severely impaired autonomic blood pressure control)

• patients who have suffered MI, stroke, life-threatening arrhythmia, or coronary revascularization within the last 6 months; patients with resting hypotension (blood pressure less than 90/50 mm Hg) or hypertension (blood pressure greater than 170/100 mm Hg); patients with unstable angina, angina with sexual intercourse, or New York Heart Association Class 2 or greater congestive heart failure; patients with known hereditary degenerative retinal disorders, including retinitis pigmentosa (use not recommended)

• patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis, or Peyronie's disease); patients who have conditions that may predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia); patients with bleeding disorders or active peptic ulceration

• concurrent use of alpha blockers or other antihypertensives or substantial amounts of alcohol

• elderly patients

• women (not indicated)

• children younger than age 18 (safety and efficacy not established).

Administration

☞ Don't give concurrently with nitrates. In a patient who has taken this drug, where nitrate administration is deemed medically necessary in a life-threatening situation, allow at least 12 hours to elapse after the last dose of avanafil before considering nitrate administration. In such circumstances, administer nitrates under close medical supervision with appropriate hemodynamic monitoring.

Use Cautiously in: Serious underlying cardiovascular disease or conditions in which sexual activity is not advised;History of sudden severe vision loss or non-arteritic ischemic optic neuropathy (NAION); may ↑ risk of recurrence;Alpha adrenergic blockers (patients should be on stable dose of alpha blockers before treatment, initiate with 50 mg dose);Anatomic penile deformity (angulation, cavernosal fibrosis, Peyronie disease);Conditions associated with priapism (sickle cell anemia, multiple myeloma, leukemia);Concurrent moderate inhibitors of the CYP3A4 enzyme system (initiate with 50 mg dose);History of hearing loss;Bleeding disorders or peptic ulceration; Geriatric: Elderly may be more sensitive to drug effects;Not intended for use in women; Pediatric: Safe use in children <18 yr not established.

Adverse Reactions/Side Effects

Central nervous system

headache (most frequent)

dizziness

Ear, Eye, Nose, Throat

nasal congestion

nasopharyngitis

sudden hearing/vision loss

Genitourinary

priapism

Dermatologic

flushing (most frequent)

Musculoskeletal

back pain

Interactions

Drug-Drug interaction

Blood levels and effects may be ↑ by CYP3A4 inhibitors, concurrent use of strong CYP3A4 inhibitors including atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, saquinavir, and telithromycin is contraindicated.A similar but lesser effect is expected with moderate CYP3A4 inhibitors including erythromycin, aprepitant, diltiaziem. fluconazole, fosamprenavir, ritonavir and verapamil ; initial dose should not exceed 50 mg/24 hr.↑ risk of hypotension with nitrates, alpha-adrenergic blockers, antihypertensives and alcohol (more than 3 units); concurrent use with nitrates is contraindicated, dosage adjustments may be necessary with others.If nitrates are medically necessary, at 12 hr should pass following avanafil adminitration.

Implementation

Patient/Family Teaching

Instruct patient to take avanafil as needed for ED at least 30 min before sexual activity and not more than once per day. Inform patient that sexual stimulation is required for an erection to occur after taking avanafil.

Advise patient that avanafil is not indicated for use in women.

Caution patient not to take avanafil concurrently with alpha adrenergic blockers (unless on a stable dose) or nitrates. If chest pain occurs after taking avanafil, instruct patient to seek immediate medical attention.

Instruct patient to notify health care professional promptly if erection lasts longer than 4 hr, if they are not satisfied with their sexual performance, develop unwanted side effects or if they experience sudden or decreased vision loss in one or both eyes or loss or decrease in hearing, ringing in the ears, or dizziness.

Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications that may interact with avanafil.

Inform patient that avanafil offers no protection against sexually transmitted diseases. Counsel patient that protection against sexually transmitted diseases and HIV infection should be considered.

has entered into a Commercial Supply Agreement with Sanofi Chimie ("Sanofi"), a wholly owned subsidiary of Sanofi, to manufacture and supply the active pharmaceutical ingredient (API) for avanafil on an exclusive basis in the United States and other territories and on a semi-exclusive basis in the European Union and Latin America.

The investigational pipeline includes: Qnexa, for which a Phase 2 study has been completed for the treatment of obesity; ALISTA, for which a Phase 2B program is ongoing for the treatment of Female Sexual Arousal Disorder (FSAD); Testosterone MDTS, for which a Phase 2 program has been completed for the treatment of Hypoactive Sexual Desire Disorder; Evamist, for which a Phase 3 program has been completed for the treatment of menopausal symptoms; avanafil, for which a Phase 2 program has been completed for the treatment of erectile dysfunction (ED); and, MUSE, which is approved and currently on the market for the

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